CAS NO: | 635323-95-4 |
生物活性 | F-15599 is a highly selective G-protein biased5-HT1A receptoragonist, withKiof 3.4 nM. | ||||||||||||||||
IC50& Target |
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体内研究 (In Vivo) | F15599 (0.06 or 0.12 mg/kg) significantly reduces l-DOPA-induced dyskinesia (LID), without affecting motor performance of rats. Rats treated with F15599 manifest less LID and mild 5-HT syndrome with the high dose of 30 μg/μL[1]. F15599 (0.0625, 0.125, 0.25, 0.5 and 1.0 mg/kg, i,p,) results in a significant and dose-dependent (MED = 0.125 mg/kg) delay in the latency to attack, and a potent reduction (ID50 = 0.095 mg/kg) in the amount of aggressive behaviour directed towards the intruder rat. Starting from the 0.25 mg/kg dose, F15599 induces clear signs of the so-called serotonin syndrome characterized by flat body posture, head-waving, lower lip retraction and hindlimb abduction, leading to increased behavioural inactivity scores and social disengagement[2]. F15599 increases the discharge rate of pyramidal neurones in medial prefrontal cortex (mPFC) from 0.2 μg/kg i.v and reduces that of dorsal raphe 5-hydroxytryptaminergic neurones at doses >10-fold higher (minimal effective dose 8.2 μg/kg i.v.). F15599 increases dopamine output in mPFC (an effect dependent on the activation of postsynaptic 5-HT1A receptors) with an ED50of 30 μg/kg i.p., whereas it reduces hippocampal 5-HT release (an effect dependent exclusively on 5-HT1A autoreceptor activation) with an ED50of 240 μg/kg i.p[3]. | ||||||||||||||||
分子量 | 394.85 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H21ClF2N4O | ||||||||||||||||
CAS 号 | 635323-95-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 250 mg/mL(633.15 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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